Month: July 2021

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.694499-26-8,4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.

694499-26-8, 3-Iodo-4-methy1-N-(4-((4-methy1piperazin-1-y1)methy1)-3-(trfluoromethy1)pheny1)Benzamide: 3-Iodo-4-methylbenzoyl chloride (0.48 g, 1.7 mmol), prepared from the reaction of3-iodo-4-methylbenzoic acid and SOCI2 (as previously described), was added to a solution of 4-((4-methylpiperazin-1 -yl)methyl)-3-(trifluoromethyl)aniline (0.47 g, 1.7 mmol), N,N5 diisopropylethylamine (0.26 g, 2.0 mmol), and a catalytic amount of DMAP in THF (10 mL).After stirring at rt for 2 h, the reaction was quenched with water. EtOAc was added and the layers separated. The combined organic layers were concentrated to dryness and purified by silica gel chromatography (eluted with 5% MeOH/DCM, MeOH was pre-saturated with ammonia gas), to provide 0.51 g of product as an off-white solid.

694499-26-8 4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 46838908, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; ARIAD PHARMACEUTICALS, INC.; GOZGIT, Joseph, M.; RIVERA, Victor, M.; SHAKESPEARE, William, C.; ZHU, Xiaotian; DALGARNO, David, C.; WO2013/162727; (2013); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

20327-23-5, 1-Cyclopropylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 3 (General procedure A); 2-(4-Cyclopropylpiperazin-1-yl)-6-methoxybenzothiazole, hydrochloride; A mixture of 2-chloro-6-methoxybenzothiazole (0.20 g, 1.0 mmol) and 1-cyclopropyl- piperazine (0.25 g, 2.0 mmol) was stirred at 120 0C overnight. The reaction mixture was allowed to cool and dissolved in a mixture of ethyl acetate a NaHCO3 solution. The phases were separated and the organic phase was washed with water (3 x) and then extracted with 0.25 M hydrochloric acid (20 ml_). The acidic aqueous extract was concentrated and re- evaporated with ethanol. The residue was crystallized from a mixture of ethanol and ethyl acetate to give 60 mg (18 %) of 2-(4-cyclopropylpiperazin-1-yl)-6-methoxybenzothiazole, hydrochloride. 1H-NMR (400MHz, DMSO-d6) delta 11.3 (brs, 1 H), 7.48 (d, 1 H), 7.45 (d, 1 H), 6.93 (dd, 1 H), 4.18-4.06 (m, 2H), 3.89-3.75 (m, 5H), 3.68-3.52 (m, 2H), 3.44-3.33 (m, 2H), 2.94-2.86 (m, 1 H), 1.21-1.15 (m, 2H), 0.85-0.79 (m, 2H).

20327-23-5, 20327-23-5 1-Cyclopropylpiperazine 4742004, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; NOVO NORDISK A/S; WO2007/110364; (2007); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

1235865-77-6, 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoic acid (5) was synthesized by the method reported. [Nat Med. 2013, 19(2): 202-8] To a solution of compound 5 (100 mg, 0.175 mmol) in anhydrous dichloromethane, compound 4g (68 mg, 0.175 mmol), EDCI (167 mg, 0.875 mmol) and DMAP (25.6 mg, 0.21 mmol) were added. Afterwards, the mixture solution was stirred for 24 h at room temperature. Completion of the reaction was confirmed by TCL. The reaction mixture was washed with HCl (1 M), NaHCO3 saturated solution and brine, concentrated and purified to afford 6g (160 mg, 85% yield) as a yellow solid.

1235865-77-6, As the paragraph descriping shows that 1235865-77-6 is playing an increasingly important role.

Reference：
Article; Zhou, Ruolan; Fang, Shaoyu; Zhang, Minmin; Zhang, Qingsen; Hu, Jian; Wang, Mingping; Wang, Chongqing; Zhu, Ju; Shen, Aijun; Chen, Xin; Zheng, Canhui; Bioorganic and Medicinal Chemistry Letters; vol. 29; 3; (2019); p. 349 – 352;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

655225-01-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.655225-01-7,tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

The compound obtained in Example 35-2 (74 mg, 0.55 mmol) was dissolved in DMF (1.5 ml). There to cesium carbonate (214 mg, 0.66 mmol), tertiaryButyl 4- (2-bromomethyl) piperazine-1-Carboxylate(323 mg, 1.1 mmol), potassium iodide (183 mg, 1.1 mmol) and stirred overnight at 70 ° C. was added a. After the reaction, the solvent was evaporated. The residue was purified by silica gel column chromatography (Chromatorex NH 20 g, hexane / ethyl acetate) to give the title compound (184 mg, 96.3percent) as a yellow oil.

655225-01-7 tert-Butyl 4-(2-bromoethyl)piperazine-1-carboxylate 15946441, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Yakult Honsha Co., Ltd.; University of Occupational and Environmental Health; Ono, Masahiro; Kobayashi, Tsuneyuki; Yamazaki, Ryuta; Haibara, Hirotake; Nishiyama, Yukiko; Hokkyo, Atsuko; Nishiyama, Hiroyuki; Kurita, Akinobu; Matsuzaki, Ken; Kono, Kimitoshi; Izumi, Hiroto; (215 pag.)JP2016/124812; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.75336-86-6,(R)-2-Methylpiperazine,as a common compound, the synthetic route is as follows.

Example 25 2-(2,8-dimethylimidazo[l,2-b]pyridazin-6-yl)-9-methyl-7-[(3R)-3-methylpiperazin-l- yl]pyrido[l,2-a]pyrimidin-4-one In a sealed tube, 2-(2,8-dimethylimidazo[l,2-b]pyridazin-6-yl)-7-fluoro-9-methyl- pyrido[l,2-a]pyrimidin-4-one (Intermediate 4; 50 mg, 0.155 mmol) and (R)-2-methylpiperazine (62 mg, 0.619 mmol, 4.0 eq.) were stirred in DMSO (2 mL) at 125C overnight. The solvent was removed under high vacuum. The residue was taken up in CH2CI2 and washed with an aqueous saturated solution of NaHC03. The organic layer was separated and dried over Na2S04 and concentrated in vacuo. The crude was purified by column chromatography (S1O2, CH2Cl2/MeOH=95/5 to 90/10) to afford the title product (40 mg, 70%) as a light yellow solid. MS m/z 404.3 [M+H+].

75336-86-6, As the paragraph descriping shows that 75336-86-6 is playing an increasingly important role.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; PTC THERAPEUTICS INC.; RATNI, Hasane; GREEN, Luke; NARYSHKIN, Nikolai A.; WEETALL, Marla L.; (80 pag.)WO2015/173181; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.161357-89-7,1-(Methylsulfonyl)piperazine hydrochloride,as a common compound, the synthetic route is as follows.

Example 2 6-(4-Methanesulfonyl-piperazin-l-vI)-2-morphoHn-4-yl-[4,5’lbipyriinidinyl-2′-ylamine (4) A mixture of Intermediate Al (198mg), Intermediate G (230mg) and potassium carbonate (293mg) was stirred in acetonitrile (10ml) at room temperature. After 24 hours the reaction mixture was diluted with ethyl acetate, washed with water, dried (MgSO4) and the solvent removed in vacuo. The residue was recrystallised from ethyl acetate/hexane to yield 4-[4-chloro-6-(4-methanesulfonyl-piperazin-l-yl)-yrimidin-2- yl]-morpholine (206mg). Reaction of 4-[4-chloro-6-(4-methanesulfonyl-piperazin- 1 -yl)-yrimidin-2-yl]- morpholine with 2-aminopyrimidine-5-boronic acid, pinacol ester using standard Suzuki conditions yielded the desired title compound. IH NMR (400MHz, CDCl3) 2.80 (3H,s), 3.28-3.24 (4H,m), 3.82-3.75 (12H,m), 5.20 (2H,s,br.), 6.16 (lH,s), 8.91 (2H,s)., 161357-89-7

The synthetic route of 161357-89-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; WO2009/66084; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.34334-28-6,4-(4-Methylpiperazin-1-yl)benzonitrile,as a common compound, the synthetic route is as follows.

Under nitrogen, 4- (4-methylpiperazin-1-yl) benzonitrile (500 mg, 2.48 mmol) and tetraisopropyl titanate (1.25 mL, 4.22 mmol) were added to ether (10 mL). Ethylmagnesium bromide (1.82 mL, 5.46 mmol, 3M ether solution) was added dropwise to the reaction system at 78 C.The reaction was stirred at room temperature for 1.5 hours.Boron trifluoride ether (0.94 mL, 7.45 mmol) was then dropped into the reaction system, and the reaction system was stirred at room temperature for 1 hour.The reaction solution was quenched with water, the reaction solution was extracted with ethyl acetate, the organic phase was separated, and the residue was purified by silica gel column chromatography (dichloromethane / methanol = 95/5) to obtain 1- (4- (4-methylpiperazine). Azin-1-yl) phenyl) cyclopropylamine (7A, 180 mg, yield: 31%) was a yellow oil., 34334-28-6

As the paragraph descriping shows that 34334-28-6 is playing an increasingly important role.

Reference：
Patent; Shanghai Dinuo Pharmaceutical Technology Co., Ltd.; Zhao Zhiming; (42 pag.)CN110467629; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

21655-48-1, cis-2,6-Dimethylpiperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

0.44 ml of ethyl 4-fluorobenzoate was dissolved in 8 ml of dimethylsulfoxide, 1.370 g of (2S, 6R) -dimethylpiperazine was added,The temperature was raised to 120 C under argon protection, and the mixture was heated for 28 hours. After heating, the reaction solution was diluted with 40 ml of water,Ethyl ester extraction, organic phase after the merger with saturated aqueous sodium chloride solution washed five times, anhydrous sodium sulfate drying, filtration concentrated, residualThe residue was chromatographed (dichloromethane: methanol = 99: 1-97: 3, V / V) to give 0.730 g of a brown oil in a yield of 92.8%., 21655-48-1

21655-48-1 cis-2,6-Dimethylpiperazine 6950261, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Duan Wenhu; Geng Meiyu; Zhao Bin; Ding Jian; Ai Jing; Fan Jun; Peng Xia; Yan Wei; Chen Yi; (77 pag.)CN106146493; (2016); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

630125-91-6, 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

630125-91-6, To a solution 4-(2-(cyclopropanecarboxamido)thiazolo[4,5-b]pyrazin-6- yl)benzoic acid (50 mg, 0.15 mmol) in DMF (1.0 mL) was added N, N- diisopropylethylamine (70 muL, 0.44 mmol), 2-(lH-7-azabenzotriazol-l-yl)-l, 1,3,3- tetramethyl uronium hexafluorophosphate methanaminium (112 mg, 0.29 mmol) and A- ((4-ethylpiperazin-l-yl)methyl)-3-(trifluoromethyl)aniline (51 mg, 0.17 mmol). The reaction mixture was stirred at room temperature for 16 h. The crude product was diluted with DMSO (1 mL) and purified by preparative reverse-phase HPLC (acetonitrile/water gradient) to give the title compound as a TFA salt. 1H NuMR 600 MHz (DMSO-J6) delta 13.21 (s, IH), 10.65 (s, IH), 9.56 (bs, IH), 9.29 (s, IH), 8.36 (J, J= 7.2, IH), 8.24 (s, IH), 8.13 (m, 3H), 7.72 (J, J= 7.8 Hz, IH), 3.69 (s, 2H), 3.46 (m, 2H), 3.13 (m, 2H), 2.98 (m, 4H), 2.40 (m, 2H), 2.06 (m, IH), 1.19 (m, 3H), 1.02 (m, 4H), MS m/z : 610.25 (M + 1).

The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; NOVARTIS AG; CHOI, Hwan, Geun; SIM, Taebo; GRAY, Nathanael; ZHOU, Wenjun; CHANG, Jae, Won; ZHANG, Jianming; WEISBERG, Ellen; WO2010/144909; (2010); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

278788-66-2, (R)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step D: (3S,9aR)-3-(3-Cyano-4-fluoro-2-methyl-phenyl)-3-hydroxy-hexahydro-pyrazino[2, 1-cli 1,4loxazine-8-carboxylic acid tert-butyl ester: Diisopropylethylamine (156 mL, 894 mmol)was added to a stirred, room temperature mixture of 3-(2-Bromo-acetyl)-6-fluoro-2-methyl-benzonitrile (176 g, 688 mmol) and (R)-4-N-Boc-2-hydroxymethyl-piperazine (149 g, 688 mmol)in THE (3500 mL) and the mixture was stirred at room temperature for 18 h. The reaction wasdiluted with 3 L EtOAc, washed 2x with 1500 mL 10% wlw NaHCO3 aqueous solution, dried over Mg504, filtered and concentrated. The residue was purified by column chromatography on silica gel (40-80% EtOAc/Hexanes, linear gradient), to provide the title compound, 278788-66-2

As the paragraph descriping shows that 278788-66-2 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; PASTERNAK, Alexander; DEJESUS, Reynalda, Keh; FRIE, Jessica, L.; PIO, Barbara; TANG, Haifeng; WALSH, Shawn, P.; WO2014/99633; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics